Levalbuterol (10 μM; 24 hours) causes 11β-HSD1 mRNA expression in airway epithelial cells, but not 11β-HSD2 expression[1].
Levalbuterol (10 μM; 24 hours) increases GRE activation in an 11β-HSD1 dependent manner in a transformed mouse airway epithelial cell line, while significantly reducing both LPS- and TNF-α-induced NF-κB activity[1].

Levalbuterol (subcutaneous injection; 1 mg/kg; 14 days) dramatically reduces pulmonary inflammation in OVA mice, as evidenced by a drop in IgE and eosinophilia[3].

Cell Line: Murine Club (MTCC) cells
Concentration: 10 μM
Incubation Time: 24 hours
Result: Increased 11β-HSD1 mRNA expression selectively.

C57BL/6 female mice with a pulmonary allergic model
1 mg/kg
Subcutaneous injection; 1 mg/kg; 14 days

Absorption, Distribution and Excretion
Inhalation delivers the drug directly to the airways and lungs, reducing systemic absorption and minimizing side effects. It is excreted in the urine. Metabolism/Metabolites Pure (R)-salbutamol, i.e., levosabutamol, is metabolized in the intestine 12 times faster than (S)-salbutamol. Biological Half-Life 3.3 - 4 hours

Effects During Pregnancy and Lactation
◉ Overview of Drug Use During Lactation
Levosalbutamol is the R-enantiomer of the β2-adrenergic agonist salbutamol (Ventolin). While there is currently no publicly available data on oral or inhaled levsalbutamol during lactation, data on the related drug terbutaline suggest that very small amounts are expected to be excreted into breast milk. Authors of multiple reviews and expert guidelines agree that the use of such drugs during lactation is acceptable due to the low bioavailability of inhaled bronchodilators and the low maternal serum concentrations after administration.
◉ Effects on Breastfed Infants
No published information found as of the revision date.
◉ Effects on Lactation and Breast Milk
No published information found as of the revision date.

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Protein Binding
Plasma protein binding is relatively low.

[1]. Anti-inflammatory effects of levalbuterol-induced 11β-hydroxysteroid dehydrogenase type 1 activity in airway epithelial cells.Front Endocrinol (Lausanne). 2015 Jan 12;5:236.

[2]. (R)-albuterol decreases immune responses: role of activated T cells.Respir Res. 2008 Jan 14;9:3.

(R)-Salbutamol is a type of salbutamol. Levosalbutamol, or levosabutamol, is a short-acting β2-adrenergic receptor agonist used to treat asthma and chronic obstructive pulmonary disease (COPD). Salbutamol was previously marketed as a racemic mixture, but its β2-agonist activity was almost entirely present in the (R)-enantiomer. The enantioselective distribution of salbutamol and the potential adverse effects of (S)-salbutamol prompted the development of an enantiomerically pure (R)-salbutamol formulation, namely levosabutamol. Levosalbutamol is a β2-adrenergic agonist. The mechanism of action of levosabutamol is as a β2-adrenergic receptor agonist. Levosalbutamol is a short-acting sympathomimetic β2-adrenergic receptor agonist with bronchodilatory effects. Levosalbutamol binds to β2-adrenergic receptors in bronchial smooth muscle, activating intracellular adenylate cyclase, which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP). Increased cAMP levels lead to activation of protein kinase A, which in turn inhibits myosin phosphorylation and reduces intracellular calcium ion concentration, ultimately resulting in bronchial smooth muscle relaxation. Increased cAMP concentration also inhibits the release of inflammatory mediators, especially those from mast cells.
R-isomer of salbutamol.
See also: Levosalbutamol hydrochloride (salt form); Levosalbutamol tartrate (salt form); Levosalbutamol sulfate (salt form)...See more...

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Drug Indications
Indications for the treatment of chronic obstructive pulmonary disease (COPD) and asthma.

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Mechanism of Action
β2-adrenergic receptors on airway smooth muscle are coupled to Gs protein. L-salbutamol activates these receptors, which in turn activates adenylate cyclase, leading to an increase in intracellular 3',5'-cyclic adenosine monophosphate (cAMP) concentration. Increased cAMP levels activate protein kinase A, which inhibits myosin phosphorylation, thereby reducing intracellular calcium ion concentration and inducing muscle relaxation. Elevated cAMP levels are also associated with inhibiting the release of mediators from airway mast cells, which may help alleviate asthma attacks.

C₁₃H₂₁NO₃

239.31

239.152

34391-04-3

Levalbuterol hydrochloride; 50293-90-8; Levalbuterol tartrate; 661464-94-4

123600

Typically exists as solid at room temperature

1.2±0.1 g/cm3

433.5±40.0 °C at 760 mmHg

159.5±17.9 °C

0.0±1.1 mmHg at 25°C

1.566

0.01

4

4

5

17

227

1

CC(C)(C)NC[C@@H](C1=CC(=C(C=C1)O)CO)O

NDAUXUAQIAJITI-LBPRGKRZSA-N

InChI=1S/C13H21NO3/c1-13(2,3)14-7-12(17)9-4-5-11(16)10(6-9)8-15/h4-6,12,14-17H,7-8H2,1-3H3/t12-/m0/s1

4-[(1R)-2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol

Levalbuterol; (R)-albuterol; Xopenex; R-albuterol; Levosalbutamol

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)